Target General Information
Target ID T31391 Target Info
Target Name Dipeptidyl peptidase 4 (DPP-4)
Synonyms Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP
Target Type Successful Target
Gene Name DPP4
Biochemical Class Peptidase
UniProt ID
Patent(s) and the Corresponding Patented Drug(s)
World Intellectual Property Organization (WIPO)
Patent ID WO2014061031
Title 2-Phenyl-5-Heterocyclyl-Tetrahydro-2H-Pyran-3-Amine Compounds for Use In The Treatment of Diabetes and Its Associated Disorders.
Abstract The present invention relates to novel compounds of the general formula (I) their tautomeric forms, their enantiomers, their diastereoisomers, their pharmaceutically accepted salts, or pro-drugs thereof, which are useful for the treatment or prevention of diabetes mellitus (DM), obesity and other metabolic disorders. The invention also relates to process for the manufacture of said compounds, and pharmaceutical compositions containing them and their use.
Applicant(s) Cadila Healthcare Limited
Representative Drug(s) D06PIP Drug Info IC50 < 10 nM Click to Show More [1]
2 D0A6LI Drug Info IC50 < 10 nM [1]
Patent ID WO2014017474
Title Collagen Peptide Composition Production Method, Dpp-4 Inhibitor, and Antihyperglycemic Agent.
Abstract Provided are a novel collagen peptide composition production method, as well as a DPP-4 inhibitor and an antihyperglycemic agent containing said collagen peptide composition. This peptide composition including a peptide represented by X-Hyp-Gly (where, X is an amino acid residue other than Gly, Hyp, and Pro) is generated by adding and dissolving ginger rhizome-derived enzymes in a collagen and/or gelatin solution. The collagen peptide composition thus obtained exhibits high DPP-4 inhibitory activity, and an excellent antihyperglycemic effect.
Applicant(s) Nippi Co., Ltd
Representative Drug(s) D0J4KQ Drug Info IC50 = 0.008 mg/ml Click to Show More [1]
2 D0BY2H Drug Info IC50 = 0.039 mg/ml [1]
Patent ID WO2014000629
Title Hexahydropentaleno Derivatives, Preparation Method and Use In Medicine Thereof.
Abstract The invention relates to hexahydropentaleno derivatives, the preparation method and use in medicine thereof, and in particular to hexahydropentaleno derivatives or stereo-isomers or pharmaceutically acceptable salts thereof as shown in general formula (I), and to the preparation method therefor and pharmaceutical compositions comprising the derivatives, and to the use thereof as a therapeutical agent, especially as a DPP-IV inhibitor. The definition of each substituent in formula (I) is the same as the definition in the description.
Applicant(s) Sunshine Lake Pharma Co., Ltd
Representative Drug(s) D0G3IL Drug Info IC50 = 1.56 nM Click to Show More [1]
2 D0KR7R Drug Info IC50 = 1.73 nM [1]
Patent ID WO2013133031
Title Dipeptidyl Peptidase-Iv Inhibitor.
Abstract Provided are a superior dipeptidyl peptidase-IV inhibitor and the like.Specifically provided are a dipeptidyl peptidase-IV inhibitor, a hypoglycemic agent and a vascular endothelial dysfunction inhibitor, each comprising, as an active ingredient, one or more peptides selected from among peptides comprising one of the amino acid sequences represented by (a)-(d): (a) Ser-Pro-Ala-Gln (SEQ ID NO: 1), (b) Gly-Pro-Val-Arg (SEQ ID NO: 2), (c) His-Pro-His-Pro-His (SEQ ID NO: 3), and (d) Ala-Pro-Lys (SEQ ID NO: 4).Also provided are new peptides comprising any one of the amino acid sequences represented by (a)-(c): (a) Ser-Pro-Ala-Gln (SEQ ID NO: 1), (b) Gly-Pro-Val-Arg (SEQ ID NO: 2), and (c) His-Pro-His-Pro-His (SEQ ID NO: 3).
Applicant(s) Morinaga Milk Industry Co
Representative Drug(s) D05LJQ Drug Info Inhibitory activity = 1900 ng/ml Click to Show More [1]
2 D04XXF Drug Info IC50 = 10500 ng/ml [1]
Patent ID WO2012089127
Title Certain Dipeptidyl Peptidase Inhibitors.
Abstract Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
Applicant(s) Shanghai Fochon Pharmaceutical Co Ltd
Representative Drug(s) D0PM4N Drug Info IC50 = 0.5 nM Click to Show More [1]
2 D0O6SK Drug Info IC50 = 0.7 nM [1]
Patent ID WO2012089123
Title Certain Dipeptidyl Peptidase Inhibitors.
Abstract Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
Applicant(s) Shanghai Fochon Pharmaceutical Co Ltd
Representative Drug(s) D02SUS Drug Info IC50 = 0.9 to 1 nM Click to Show More [1]
2 D04UXC Drug Info IC50 = 0.9 to 1 nM [1]
3 D0KS8Y Drug Info IC50 = 0.9 to 1 nM [1]
Patent ID WO2012088680
Title Certain Dipeptidyl Peptidase Inhibitors.
Abstract Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
Applicant(s) Shanghai Fochon Pharmaceutical Co Ltd
Representative Drug(s) D02SUS Drug Info IC50 = 0.9 to 1 nM Click to Show More [1]
2 D04UXC Drug Info IC50 = 0.9 to 1 nM [1]
3 D0KS8Y Drug Info IC50 = 0.9 to 1 nM [1]
Patent ID WO2014018355
Title Treating Diabetes with Dipeptidyl Peptidase-Iv Inhibitors.
Abstract The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0XB0Q Drug Info IC50 = 8.8 nM [1]
Patent ID WO2013065832
Title Dpp-4 Inhibitor.
Abstract A DPP-4 inhibitor containing, as an active ingredient, a peptide represented by formula (1): Xe-Pro/Ala/Hyp-Xa-Xb-Xc-Xd (wherein Xe represents an amino acid residue having an isoelectric point of 5.9-6.3; Pro/Ala/Hyp represents Pro, Ala or Hyp; Xa represents an amino acid residue other than Hyp, Pro and Arg or a deletion; Xb represents Gly, Pro or a deletion; Xc represents Pro, Ala or a deletion; and Xd represents an amino acid residue or a deletion). This inhibitor is expected to exert an activity of decreasing a blood glucose level through the potentiation of the activity of an incretin, and therefore can be used as a therapeutic agent for diabetes. In addition, this inhibitor can act on an immune system or the like, and therefore can be used for the treatment of skin diseases or the like.
Applicant(s) Nippi Co., Ltd
Representative Drug(s) D0WE8K Drug Info IC50 = 60 nM [1]
Patent ID WO2013010964
Title Substituted Quinazolines, The Preparation Thereof and The Use Thereof In Pharmaceutical Compositions.
Abstract The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D05HLQ Drug Info IC50 = 6 pM [1]
Patent ID WO2013006526
Title Tricyclic Heterocycles Useful As Dipeptidyl Peptidase-Iv Inhibitors.
Abstract The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0E8AS Drug Info IC50 = 1.7 nM [1]
Patent ID WO2012147092
Title Novel Salts of Dpp-Iv Inhibitor.
Abstract The present invention discloses new salts of (2R)-4-oxo-4-[3-(trifluoromethyl)- 5,6-dihydro[ l,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]- l -(2,4,5-trifluorophenyl)butan-2- amine i.e. gentisate, adipate and trifluoro acetic acid salts. The invention also describes the new. crystalline and amorphous forms of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro[ l,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]- l -(2,4,5-triflLiorophenyl)butan-2-amine gentisate. The present invention also discloses novel crystalline salt form of (2R)-4-oxo-4-[3- (trifliioromethyl)-5,6-dihydiO[ 1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]- 1 -(2,4,5- trifluorophenyl)butan-2-amine hydrochloride and novel crystalline and amorphous salt forms of besylate and process for their preparation and isolation.
Applicant(s) Cadila Healthcare Limited
Representative Drug(s) D0JP6A Drug Info IC50 = 18 nM [1]
Patent ID WO2012089122
Title Certain Dipeptidyl Peptidase Inhibitors.
Abstract Provided are compounds represented by formula (I), their pharmaceutical compositions, and their uses for preparing medicaments as inhibitors of dipepetidyl peptidase-IV enzyme, wherein each substitutuent of formula (I) is defined as the description.
Applicant(s) Shanghai Fochon Pharmaceutical Co Ltd
Representative Drug(s) D0UV3I Drug Info IC50 = 0.5 nM [1]
Patent ID WO2012088677
Title Certain Dipeptidyl Peptidase Inhibitors.
Abstract Disclosed are compounds represented by formula (I) and their pharmaceutical compositions, and uses thereof in the preparation of the drugs for treating a condition responsive to inhibition of dipeptidyl peptidase-IV enzyme, wherein each substituent of formula (I) is defined as the description.
Applicant(s) Shanghai Fochon Pharmaceutical Co Ltd
Representative Drug(s) D0UV3I Drug Info IC50 = 0.5 nM [1]
Patent ID WO2012078448
Title Tricyclic Heterocycles Useful As Dipeptidyl Peptidase-Iv Inhibitors.
Abstract The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. I.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0K2ZQ Drug Info IC50 = 0.38 nM [1]
Patent ID WO2014034626
Title Crystal of N-[2-({2-[(2S)-2-Cyanopyrrolidin-1-Yl]-2- Oxoethyl}Amino)-2-Methylpropyl]-2-Methylpyrazolo[1,5-A]Pyrimidine-6-Carboxamide.
Abstract [Problem] To provide: a crystal of anagliptin, which has high purity, excellent stability, low hygroscopicity and a property of being dissolved in water extremely satisfactorily; and a method for producing the crystal of anagliptin. [Solution] A crystal of anagliptin, which has peaks at points located adjacent to diffraction angles, each of which is expressed in 2, of 9.8, 17.4, 18.6, 25.3 and 25.8 and has substantially the same powder X-ray diffraction pattern as that illustrated in fig. 1. The crystal can be produced by reacting N-(2-amino-2-methylpropyl)-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide with (2S)-N-chloroacetyl- 2-cyanopyrrolidine in an organic solvent, then purifying the resultant product by column chromatography to produce an amorphous form of anagliptin, and then crystallizing the amorphous form of anagliptin from 2-propanol.
Applicant(s) Sanwa Chemistry Laboratory Co., Ltd
Representative Drug(s) D06GQG Drug Info N.A. [1]
Patent ID WO2014018350
Title Treating Diabetes with Dipeptidyl Peptidase-Iv Inhibitors.
Abstract The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0K5YJ Drug Info N.A. [1]
Patent ID WO2013111158
Title Process for The Preparation of Dpp-Iv Inhibitor.
Abstract The present invention provides a process for the preparation of (l S,3S,5S)-2-[(2S)-2- amino-2-(3 -hydroxyadamantan- l-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its pharmaceutically acceptable salts thereof, represented by the compound of formula- 1.
Applicant(s) Msn Laboratories Limited
Representative Drug(s) D01MMT Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20130184322
Title Novel dipeptidyl-peptidase-iv inhibitors.
Representative Drug(s) D0E9MO Drug Info IC50 = 1.5 nM Click to Show More [1]
2 D02LNB Drug Info IC50 = 46 nM [1]
Japan Patent Office (JPO)
Patent ID JP2013184962
Title Dipeptidyl Peptidase 4 Inhibitor.
Applicant(s) Morinaga Milk Industry Co
Representative Drug(s) D0QE8Z Drug Info IC50 = 12200 ng/ml Click to Show More [1]
2 D0B4CH Drug Info IC50 = 12500 ng/ml [1]
3 D0E8WW Drug Info IC50 = 25500 ng/ml [1]
Patent ID JP2013040111
Title Dipeptidyl Peptidase-4 Inhibitor and Method of Production of The Same.
Applicant(s) Okayama Prefecture
Representative Drug(s) D05GEY Drug Info ID50 = 410000 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN103848835
Title Dipeptidyl Peptidase 4 Inhibitor, Application Thereof, Intermediate Body Thereof and Preparation Method of Intermediate Body Thereof.
Applicant(s) Shanghai Sun-Sail Pharmaceutical Science & Technology Co
Representative Drug(s) D0P3DS Drug Info IC50 = 2.52 nM Click to Show More [1]
2 D0EL5B Drug Info IC50 = 3.51 nM [1]
Patent ID CN103772323
Title Dipepitidyl Peptidase 4 Inhibitor Compound.
Applicant(s) Nanjing Huawei Pharmaceutical Science and Technology Development Co
Representative Drug(s) D02UOW Drug Info IC50 = 0.6 to 0.8 nM Click to Show More [1]
2 D0IO0M Drug Info IC50 = 0.6 to 0.8 nM [1]
3 D0W6HL Drug Info IC50 = 0.6 to 0.8 nM [1]
Patent ID CN103626775
Title Dpp 4 Inhibitor with Diazine Structure.
Applicant(s) Nanjing Huawei Pharmaceutical Science and Technology Development Co
Representative Drug(s) D0XN3O Drug Info IC50 = 6.5 nM Click to Show More [1]
2 D0BJ2X Drug Info IC50 = 7.4 nM [1]
Patent ID CN103044392
Title Dpp 4 Inhibitor Preparation Method.
Applicant(s) Lianyungang Runzhong Pharmaceutical Co
Representative Drug(s) D04MAZ Drug Info IC50 = 0.27 nM Click to Show More [1]
2 D0CW9H Drug Info IC50 = 0.35 nM [1]
Patent ID CN103044391
Title Dpp 4 Inhibitor.
Applicant(s) Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences
Representative Drug(s) D04MAZ Drug Info IC50 = 0.27 nM Click to Show More [1]
2 D0CW9H Drug Info IC50 = 0.35 nM [1]
Patent ID CN102311448
Title Thieno-pyrimidone DPP-IV (dipeptidyl peptidase) inhibitor.
Applicant(s) Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences
Representative Drug(s) D0RT1R Drug Info IC50 = 3.1 nM Click to Show More [1]
2 D07JJT Drug Info IC50 = 3.6 nM [1]
Patent ID CN103848811
Title Uracil Derivative, Preparation Method and Application Thereof.
Applicant(s) Qilu Pharmaceutical Co
Representative Drug(s) D0G1CF Drug Info N.A. Click to Show More [1]
2 D0PF2W Drug Info N.A. [1]
3 D0T1WB Drug Info N.A. [1]
Patent ID CN103420981
Title Substituted Pyrrolidinyl Contained Thiomorpholine Compounds.
Applicant(s) Institute of Materia Medica, Chinese Academy of Medical Sciences
Representative Drug(s) D06HJX Drug Info N.A. Click to Show More [1]
2 D0D4BP Drug Info N.A. [1]
Patent ID CN102453001
Title Thiomorpholine compounds and their preparation and use.
Abstract The present invention relates to a thiomorpholine compound and its preparation method and uses. Specifically, the present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt, free base, solvate, ester, prodrug, stereoisomer, geometric isomer, racemate, wherein each symbol is as described in the specification. The present invention further relates to pharmaceutical compositions comprising a compound of the invention, the compounds of the present invention is the preparation of a medicament for the treatment and / or prophylaxis of high DPP-IV activity with DPP-IV or overexpression of a disease or condition associated in uses, and methods of using the compounds of the present invention is the treatment of related diseases. Compounds of the invention have potent inhibition of DPP-IV activity.
Applicant(s) Institute of Materia Medica, Chinese Academy of Medical Sciences
Representative Drug(s) D06HJX Drug Info N.A. Click to Show More [1]
2 D0D4BP Drug Info N.A. [1]
Patent ID CN103373999
Title Purine compounds, intermediates, preparation method and application.
Abstract The present invention discloses a xanthine compound I, R1 is hydrogen or 2-cyanophenyl; R2 is 2-cyanobenzyl group; R3 is an amino group or, where, n = 2 ~ 4, m = 2 ~ 3, D is H or NH2, E is CH2 or NH. A method for preparing xanthine compound I: compound II with the nucleophilic substitution reaction R3H; or nucleophilic compound II with R-3- tert-butyloxycarbonyl-amino-piperidine substitution reaction, de tert acyl protecting group. The present invention also discloses a xanthine compound according to any one of the intermediates I, R1, and R2 as described above. Application of a xanthine compound I in the manufacture DPP-4 inhibitor activity, or, and / or DPP-4 inhibition by drugs enzyme treatment and prevention of diseases associated therewith in. Xanthine compounds of the present invention provides a new direction for the development of DPP-4 inhibitor, is important for the development of potential DPP-4 inhibitor.
Applicant(s) Shanghai Institute of Pharmaceutical Industry
Representative Drug(s) D0ND5K Drug Info 89.5% inhibition = 1000 ng/ml [1]
Patent ID CN103788070
Title Dpp 4 Inhibitor Polymer.
Applicant(s) Nanjing Huawei Pharmaceutical Science and Technology Development Co
Representative Drug(s) D00GNP Drug Info IC50 = 0.6 nM [1]
Patent ID CN103172633
Title Compound, and Preparation Method and Application Thereof.
Applicant(s) Chengdu Diao Pharmaceutical Group Co
Representative Drug(s) D0T6SD Drug Info IC50 = 0.09 nM [1]
Patent ID CN103030631
Title Dipepitidyl Peptidase 4 Inhibitor Compound.
Applicant(s) Jiangsu Chia-Tai Tianqing Pharmaceutical Co
Representative Drug(s) D0J5EW Drug Info IC50 < 30 nM [1]
Patent ID CN103664893
Title Novel Dpp 4 Inhibitor, and Preparation Method and Medicinal Application Thereof.
Applicant(s) China Pharmaceutical University
Representative Drug(s) D0J0UN Drug Info N.A. [1]
Patent ID CN102863440
Title Crystallographic form of Salt of Dipeptidyl Peptidase 4 Inhibitor.
Applicant(s) Kbp Biomedical Co
Representative Drug(s) D0A5QV Drug Info N.A. [1]
Intellectual Property Office in India (IP India)
Patent ID IN2013254994
Title Preparation of Thienopyrimidones Derivatives As DPP-4 Inhibitors.
Applicant(s) Orchid Chemicals & Pharmaceuticals
Representative Drug(s) D0LG1I Drug Info IC50 = 100 nM [1]
Patent ID IN2012251197
Title Preparation of novel pyrrolidines as DPP-4 inhibitors.
Applicant(s) Matrix Laboratories
Representative Drug(s) D0N9CV Drug Info IC50 = 8.1 nM [1]
Intellectual Property Office of United Kingdom (IPOUK)
Patent ID GB2497351
Title Novel compounds.
Applicant(s) Prosidion Ltd
Representative Drug(s) D06PDK Drug Info IC50 < 1000 nM [1]
References
REF 1 DPP-4 inhibitors: a patent review (2012 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):209-36.

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